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AR077497A1 - SPIROCICLICAL COMPOUNDS CONTAINING NITROGEN AND ITS PHARMACEUTICAL USE - Google Patents

SPIROCICLICAL COMPOUNDS CONTAINING NITROGEN AND ITS PHARMACEUTICAL USE

Info

Publication number
AR077497A1
AR077497A1 ARP100102681A ARP100102681A AR077497A1 AR 077497 A1 AR077497 A1 AR 077497A1 AR P100102681 A ARP100102681 A AR P100102681A AR P100102681 A ARP100102681 A AR P100102681A AR 077497 A1 AR077497 A1 AR 077497A1
Authority
AR
Argentina
Prior art keywords
group
different
same
atom
following
Prior art date
Application number
ARP100102681A
Other languages
Spanish (es)
Inventor
Akimi Hori
Masafumi Inoue
Yoshinori Hara
Makoto Shiozaki
Yasunori Hase
Katsuya Maeda
Tomoya Miura
Hiroshi Yamanaka
Satoru Noji
Original Assignee
Japan Tobacco Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43529436&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR077497(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Japan Tobacco Inc filed Critical Japan Tobacco Inc
Publication of AR077497A1 publication Critical patent/AR077497A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Ophthalmology & Optometry (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Obesity (AREA)
  • Oncology (AREA)
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  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Uso farmacéutico de él en el tratamiento de rechazo de trasplante de organos, reaccion de injerto versus huésped después de trasplante, enfermedad autoinmune, enfermedad alérgica y enfermedad mieloproliferativa cronica. Reivindicacion 1: Un compuesto caracterizado por la siguiente formula general (1) en donde Ra es igual o diferente y cada uno: (1) alquilo C1-6 o (2) átomo de halogeno, n1 es un numero entero seleccionado de 0 a 4, Rb es igual o diferente y cada uno: (1) alquilo C1-6 o (2) átomo de halogeno, n2 es un numero entero seleccionado de 0 a 4, m1 es un numero entero seleccionado de 0 a 3, m2 es un numero entero seleccionado de 1 a 4, Xa=Xb es: (1) CH=CH, (2) N=CH o (3) CH=N, X es: (1) átomo de nitrogeno o (2) C-Rd, en donde Rd es átomo de hidrogeno o átomo de halogeno, Rc es un grupo seleccionado de los siguientes (1) a (6): (1) átomo de hidrogeno, (2) alquilo C1-6 opcionalmente sustituido con los mismos o diferentes 1 a 5 sustituyentes seleccionados del siguiente Grupo A, (3) -C(=O)-Rc1, (4) -C(=O)-O-Rc2, (5) -C(=O)NRc3Rc4 en donde Rc1, Rc2, Rc3 y Rc4 son iguales o diferentes y cada uno: (i) átomo de hidrogeno o (ii) alquilo C1-6 opcionalmente sustituido con los mismos o diferentes 1 a 5 sustituyentes seleccionados del siguiente Grupo A o (6) un grupo de la formula: (2) en donde Ya es un grupo seleccionado de los siguientes (i) a (iii): (i) alquileno C1-6, (ii) -C(=O)- o (iii) -C(=O)-O-, anillo T es: (i) arilo C6-10, (ii) cicloalquilo C3-10 o (iii) monoheterociclilo saturado en donde el monoheterociclilo saturado comprende 1 a 4 heteroátomos seleccionados de átomo de nitrogeno, átomo de oxígeno o átomo de azufre, así como átomos de carbono y la cantidad de átomos constituyentes del anillo es 3 a 7, Rc5 es igual o diferente y cada uno: i) ciano o (ii) nitro, p es un numero entero seleccionado de 0 a 4, Grupo A es el grupo que consiste en: (a) hidroxilo, (b) alcoxi C1-6, (c) ciano, (d) alcoxi C1-6-carbonilo, (e) alquil C1-6-carboniloxi y (f) alquenil C2-6-oxi o una de sus sales o solvatos farmacéuticamente aceptables.Pharmaceutical use of it in the treatment of organ transplant rejection, graft versus host reaction after transplant, autoimmune disease, allergic disease and chronic myeloproliferative disease. Claim 1: A compound characterized by the following general formula (1) wherein Ra is the same or different and each: (1) C1-6 alkyl or (2) halogen atom, n1 is an integer selected from 0 to 4 , Rb is the same or different and each: (1) C1-6 alkyl or (2) halogen atom, n2 is an integer selected from 0 to 4, m1 is an integer selected from 0 to 3, m2 is a integer selected from 1 to 4, Xa = Xb is: (1) CH = CH, (2) N = CH or (3) CH = N, X is: (1) nitrogen atom or (2) C-Rd , wherein Rd is hydrogen atom or halogen atom, Rc is a group selected from the following (1) to (6): (1) hydrogen atom, (2) C1-6 alkyl optionally substituted with the same or different 1 to 5 substituents selected from the following Group A, (3) -C (= O) -Rc1, (4) -C (= O) -O-Rc2, (5) -C (= O) NRc3Rc4 where Rc1, Rc2, Rc3 and Rc4 are the same or different and each: (i) hydrogen atom or (ii) C1-6 alkyl optionally substituted with the same or different 1 to 5 substituents selected from the following Group A or (6) a group of the formula: (2) where It is already a group selected from the following (i) to (iii): (i) C1-6 alkylene, (ii) -C (= O) - or (iii) -C (= O) -O-, T-ring is: (i) C6-10 aryl, (ii) C3-10 cycloalkyl or (iii) saturated monoheterocyclyl wherein the monoheterocyclyl saturated comprises 1 to 4 heteroatoms selected from nitrogen atom, oxygen atom or sulfur atom, as well as carbon atoms and the amount of constituent atoms of the ring is 3 to 7, Rc5 is the same or different and each: i) cyano or (ii) nitro, p is an integer selected from 0 to 4, Group A is the group consisting of: (a) hydroxyl, (b) C1-6 alkoxy, (c) cyano, (d) C1- alkoxy 6-carbonyl, (e) C1-6 alkylcarbonyloxy and (f) C2-6-oxy alkenyl or a pharmaceutically acceptable salt or solvate thereof.

ARP100102681A 2009-07-31 2010-07-23 SPIROCICLICAL COMPOUNDS CONTAINING NITROGEN AND ITS PHARMACEUTICAL USE AR077497A1 (en)

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JP2009179502 2009-07-31

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US (4) US8609647B2 (en)
EP (3) EP3181570A1 (en)
JP (9) JP5520158B2 (en)
KR (1) KR101773208B1 (en)
CN (1) CN102510865B (en)
AR (1) AR077497A1 (en)
AU (1) AU2010278066B2 (en)
BR (1) BR112012002157B1 (en)
CA (1) CA2767899C (en)
CO (1) CO6491052A2 (en)
CY (1) CY1118747T1 (en)
DK (1) DK2460806T3 (en)
ES (1) ES2616705T3 (en)
FI (1) FIC20250012I1 (en)
FR (1) FR25C1010I1 (en)
HR (1) HRP20170447T1 (en)
HU (2) HUE033070T2 (en)
IL (1) IL217048A (en)
LT (2) LT2460806T (en)
ME (1) ME02667B (en)
MX (1) MX2012001313A (en)
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NL (1) NL301321I2 (en)
NO (1) NO2025014I1 (en)
NZ (1) NZ597994A (en)
PE (1) PE20121276A1 (en)
PL (1) PL2460806T3 (en)
PT (1) PT2460806T (en)
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SG (1) SG176918A1 (en)
SI (1) SI2460806T1 (en)
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RU2618673C2 (en) 2011-12-21 2017-05-10 Цзянсу Хэнжуй Медсин Ко., Лтд. Derivatives of pyrrolopyrimidine useful as jak-kinases inhibitors
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